# US 5,708,037 A · Inhibitor of inflammatory cytokine formation comprising polyprenyl derivatives as the active ingredient > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 5,708,037 A - Document ID: US5708037A - Status: Granted - Kind: A - Application number: 08/656,576 - Filed: 1996-05-31 - Granted: 1998-01-13 - Earliest claimed: 1993-12-01 - Assignees: Sankyo Company, Limited - Inventors: Akikuni Yagita - Web page: https://patentgrep.com/patent/US5708037A ## CPC - A61K 31/235: having an aromatic ring attached to a carboxyl group - A61K 31/045: Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates - A61K 31/047: having two or more hydroxy groups, e.g. sorbitol - A61K 31/08: acyclic, e.g. paraformaldehyde - A61K 31/215: of carboxylic acids - A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate - A61K 31/22: of acyclic acids, e.g. pravastatin - A61K 31/23: of acids having a carboxyl group bound to a chain of seven or more carbon atoms - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Polyprenyl derivatives having the general formula as the active ingredient: ##STR1## where R.sup.1 and R.sup.2 are the same or different, and each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.12 aliphatic acyl group, a C.sub.7 -C.sub.11 aromatic acyl group or a C.sub.8 -C.sub.12 aryl-substituted aliphatic acyl group; and n represents an integer from 0 to 2, show excellent activity in the inhibition of the formation of inflammatory cytokines, and they exhibit an excellent therapeutic effect on inflammatory bowel diseases such as ulcerative colitis, Crohn's disease and Behcet syndrome. ## Claims ### Claim 1 A method for the prophylaxis or therapy of diseases which are amenable to the inhibition of inflammatory cytokine formation, said method comprising administering an effective amount, to a patient in need thereof, of a polyprenyl having the following formula, as the active ingredient: ##STR3## where R.sup.1 and R.sup.2 are the same or different, and each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.12 aliphatic acyl group, a C.sub.7 -C.sub.11 aromatic acyl group or a C.sub.8 -C.sub.12 aryl-substituted aliphatic acyl group; and n represents an integer from 0 to 2. ### Claim 2 (depends on 1) The method for the prophylaxis or therapy of diseases, according to claim 1, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom, a methyl group, a C.sub.2 -C.sub.12 aliphatic acyl group, a benzoyl group or a cinnamoyl group. ### Claim 3 (depends on 1) The method for the prophylaxis or therapy of diseases, according to claim 1, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom or a C.sub.2 -C.sub.6 aliphatic acyl group. ### Claim 4 (depends on 1) The method for the prophylaxis or therapy of diseases, according to claim 1, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom or an acetyl group. ### Claim 5 (depends on 1) The method for the prophylaxis or therapy of diseases, according to claim 1, in which the active ingredient is a polyprenyl derivative wherein each of R.sup.1 and R.sup.2 is a hydrogen atom. ### Claim 6 (depends on 1) The method for the prophylaxis or therapy of diseases, according to claim 1, in which the active ingredient is a polyprenyl derivative wherein n is 1. ### Claim 7 (depends on 1) The method for the prophylaxis or therapy of diseases, according to claim 1, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom or an acetyl group; and n is 1. ### Claim 8 (depends on 1) The method for the prophylaxis or therapy of diseases, according to claim 1, in which the active ingredient is a polyprenyl derivative wherein each of R.sup.1 and R.sup.2 is a hydrogen atom and n is 1. ### Claim 9 A method for the prophylaxis or therapy of ulcerative colitis, comprising administering an effective amount, to a patient in need thereof, of a polyprenyl derivatives having the following formula, as the active ingredient: ##STR4## where R.sup.1 and R.sup.2 are the same or different, and each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.12 aliphatic acyl group, a C.sub.7 -C.sub.11 aromatic acyl group or a C.sub.8 -C.sub.12 aryl-substituted aliphatic acyl group; and n represents an integer from 0 to 2. ### Claim 10 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom, a methyl group, a C.sub.2 -C.sub.12 aliphatic acyl group, a bezoyl group or a cinnamoyl group. ### Claim 11 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom or a C.sub.2 -C.sub.6 aliphatic acyl group. ### Claim 12 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom or an acetyl group. ### Claim 13 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein each of R.sup.1 and R.sup.2 is a hydrogen atom. ### Claim 14 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein n is 1. ### Claim 15 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein R.sup.1 and R.sup.2 are the same, and each represents a hydrogen atom or an acetyl group; and n is 1. ### Claim 16 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein each of R.sup.1 and R.sup.2 is a hydrogen atom and n is 1. ### Claim 17 (depends on 9) The method for the prophylaxis or therapy of ulcerative colitis according to claim 9, in which the active ingredient is a polyprenyl derivative wherein each of R.sup.1 and R.sup.2 is a hydrogen atom and n is 1.